Egolanza, pills 10mg 28pcs

Composition

1 tablet contains: Active ingredient: 10 mg of olanzapine (in the form of olanzapine dihydrochloride trihydrate, respectively, in each film-coated tablet). excipients: core: microcrystalline cellulose, lactose monohydrate, hyprolose (hydroxynropylcellulose), crospovidone, magnesium stearate. shell: hypromellose, quinoline yellow dye, opadray Y-1-7000 white: hypromellose (62.5%), titanium dioxide (31.25%), macrogol 400 (6.25% mg)

Pharmacological action

Egolanza is an antipsychotic (neuroleptic).

Olanzapine is an antipsychotic (neuroleptic) with a broad pharmacological spectrum of effects on a number of receptor systems. It has affinity for serotonin (5-HT2 A/C 5 HTZ,5 HT6), dopamine (D1, D2, D3, D4, D5), muscarinic (M1-5), adrenergic (alpha-1) and histamine (H1) receptors.

Antagonism to serotonin (5 HT), dopamine and cholinergic receptors was revealed. It has a more pronounced affinity and activity for serotonin 5 HTt receptors, in comparison with dopamine D2 receptors.

Selectively reduces the excitability of meiulimbic (A10) dopaminergic neurons, has a minor effect on the striatal (A9) nerve pathways involved in the regulation of motor functions.

Reduces the conditioned defense reflex at lower doses than those that cause catalepsy. Enhances the anti-anxiety effect during the “anxiolytic” test. Significantly reduces productive (including delusions, hallucinations) and negative symptoms.

Indications

Schizophrenia (exacerbation, maintenance and long-term anti-relapse therapy). Bipolar affective disorder (monotherapy or in combination with Li+ or valytroic acid): acute manic or mixed episodes with / without psychotic manifestations and / without rapid phase change.

Relapse of bipolar disorder and prevention of relapses of bipolar disorder (with the effectiveness of the drug in the treatment of the manic phase).

Contraindications

Hypersensitivity to the Active ingredient or any of the components of the drug. Angle-closure glaucoma. Dementia-related psychoses and/or behavioral disorders. Lactation period. Children (under 18 years of age due to insufficient clinical data). Lactose intolerance, lactase deficiency, or glucose-galactose malabsorption (the drug contains lactose).

With caution Liver failure, renal failure, prostatic hyperplasia, epilepsy, history of convulsive syndrome, myelosuppression (including leukopenia, neutropenia). myeloproliferative diseases, hypereosinophilic syndrome, paralytic intestinal obstruction, pregnancy, cardiovascular and cerebrovascular diseases or other conditions predisposing to arterial hypotension, congenital prolongation of the QT interval on the electrocardiogram (ECG) (increase in the corrected-QT interval (QTc) on the ECG), or in the beginning of conditions that can potentially cause an increase in the QT interval (for example, simultaneous use of drugs that prolong the QT interval, congestive heart failure, hypokalemia, hypomagnesemia), old age, as well as simultaneous use of other drugs of central action; immobilization.

Side effects

From the nervous system: very often – drowsiness; often-dizziness, akathisia, Parkinsonism, asthenia, dyskinesia; rarely-convulsive syndrome (more often with a history of convulsive syndrome); very rarely-dystonia (including oculogir crisis) and tardive dyskinesia. Very rarely, neuroleptic malignant syndrome (NMS) can develop. Clinical manifestations of NMS include fever, muscle rigidity, changes in mental state, instability of autonomic functions (unstable levels of heart rate and blood pressure, tachycardia, sweating, cardiac arrhythmia). Additional signs may include increased creatine phosphokinase levels, myoglobinuria (rhabdomyolysis), and acute renal failure. If the patient develops symptoms and signs of NMS or develops an unexplained fever without additional clinical manifestations of NMS, all antipsychotic agents, including olanzapine, should be discontinued.

When the drug is abruptly discontinued, symptoms such as increased sweating, insomnia, tremor, anxiety, nausea or vomiting are very rare.

From the cardiovascular system: often-hypotension (including orthostatic); infrequently-bradycardia with or without collapse; very rarely-increased QTc interval on the ECG, ventricular tachycardia/fibrillation and sudden death, very rarely-thromboembolism (including pulmonary embolism and deep vein thrombosis).

From the digestive system: often-transient anticholinergic effects, including constipation and dryness of the oral mucosa; rarely-hepatitis; very rarely-pancreatitis.

From the side of metabolism: very often-weight gain; often-increased appetite, hypertriglyceridemia; very rarely-hyperglycemia and / or decompensation of diabetes mellitus, sometimes manifested by ketoacidosis or coma, including death; hypercholesterolemia, hypothermia.

From the digestive system: often-transient, asymptomatic increase in the activity of” hepatic ” transaminases (alanine aminotransferase (ALT), aspartate aminotransferase (ACT), especially at the beginning of therapy; rarely – hepatitis (including hepatocellular, cholestatic or mixed liver damage).

From the hematopoietic organs: often-eosinophilia; rarely-leukopenia; very rarely-thrombocytopenia, neutropenia.

Musculoskeletal disorders: very rare-rhabdomyolysis.

From the genitourinary system: very rarely – urinary retention, priapism.

From the skin: rarely-skin rash, infrequently-photosensitization reactions; very rarely-alopecia.

Allergic reactions: rarely – skin rash; very rarely-anaphylactoid reactions, angioedema, pruritus or urticaria.

Other: often-asthenia, peripheral edema; very rarely-withdrawal syndrome.

Laboratory parameters: hyperprolactinemia is very common, but clinical manifestations (for example, gynecomastia, galactorrhea, and breast enlargement) are rare. In most patients, prolactin levels spontaneously normalize without discontinuation of therapy. Rarely-transient, asymptomatic increase in ALT and ACT activity. Infrequently-increased creatine phosphokinase (CPK) activity; very rarely-increased alkaline phosphatase (ALP) and total bilirubin activity. In isolated cases, there was an increase in the concentration of glucose in blood plasma, triglycerides, cholesterol, and asymptomatic eosinophilia.

In elderly patients with dementia, a high incidence of deaths and cerebrovascular disorders (stroke, transient ischemic attacks) has been recorded in studies. Gait disorders and falls were very common in this category of patients. Pneumonia, fever, lethargy, erythema, visual hallucinations, and urinary incontinence were also common.

Among patients with drug-induced (dopamine agonist-induced) psychoses associated with Parkinson’s disease, worsening of Parkinsonian symptoms and the development of hallucinations were often recorded.

There are data on the development of neutropenia (4.1%) against the background of combination therapy with valproic acid in patients with bipolar mania. Concomitant therapy with valproic acid or lithium increases the frequency (more than 10%) of tremors, dryness of the oral mucosa, increased appetite, or weight gain. Speech disorders were also recorded (from 1 to 10%).

Interaction

Inducers or inhibitors of the CYP1A2 isoenzyme can alter olanzapine metabolism. Inducers of the CYP1A2 isoenzyme: olanzapine clearance increases in smoking patients and with simultaneous use of carbamazepine, which leads to a decrease in the concentration of olanzapine in blood plasma. It may be necessary to increase the dose of the drug. CYP1A2 isoenzyme inhibitors: fluvoxamine significantly inhibits olanzapine metabolism. Reducing the clearance of olanzapine increases the Maxax of olanzapine in non-smoking women by 54% and 77% in smoking men, AUC-by 52% and 108%, respectively, therefore, in patients taking fluvoxamine or any other inhibitor of the CYP1A2 isoenzyme (for example, ciprofloxacin), the possibility of using a lower initial dose of olanzapine should be considered.

Activated charcoal reduces the bioavailability of olanzapine by 50-60% and should be taken at least 2 hours before or 2 hours after olanzapine.

Fluoxetine (a CYP2D6 inhibitor), as well as a single dose of antacids (aluminum or magnesium) or cimetidine, did not significantly affect the pharmacokinetics of olanzapine.

Ethanol did not affect the pharmacokinetics of olanzapine at steady state, however, taking ethanol together with olanzapine may be accompanied by an increase in the pharmacological effects of olanzapine (sedation).

Olanzanine slightly inhibits the formation of valproic acid glucuronide (the main pathway of metabolism). Valproic acid has little effect on olanzapine metabolism. A clinically significant pharmacokinetic interaction between olanzapine and valproic acid is unlikely.

Caution should be exercised when using olanzapine with drugs that prolong the QTc interval (amitriptyline, chlorpromazine. droperidol, thioridazine, pimozide, quinidine, procainamide, sotalol, ephedrine, epinephrine, terbutaline, erythromycin, trimethoprim / sulfamethoxazole, ketoconazole, fluconazole, etc. ) that disrupt the electrolyte balance or inhibit olanzapine metabolism in the liver.

Concomitant use of olanzapine and antiparkinsonian medications in patients with Parkinson’s disease and dementia is not recommended.

Olanzapine exhibits dopamine antagonism and, theoretically, can inhibit the action of levodopa and dopamine agonists.

Olanzapine does not inhibit major CYP450 isoenzymes in vitro (e. g.,1 A2,2D6,2C9,2C19, ZA4), and a clinically significant interaction is unlikely. No inhibition of the metabolism of the following active substances was found: tricyclic antidepressants (mainly representing the CYP2D6 pathway), warfarin (CYP2C9), theophylline (CYP1A2) or diazepam (CYP3A4 and 2C19).

No interaction was detected when co-administered with lithium or biperiden.

How to take, course of use and dosage

Inside, regardless of food intake, once – 5-20 mg/day. For schizophrenia in adults, the recommended starting dose is 10 mg / day. In acute mania associated with bipolar disorders in adults – 15 mg / day (1 time) as monotherapy or 10 mg/day (1 time) in combination with Li+ or valproic acid (maintenance therapy at the same dose).

Prevention of recurrent bipolar disorder: The recommended starting dose is 10 mg per day. Patients who have previously received olanzapine to treat a manic episode should continue treatment at the same dose to prevent relapse. In the presence of a new manic, mixed or depressive episode, olanzapine should be continued (if necessary, specifying the dose); if there are clinical indications, additional medications should be prescribed to eliminate mood disorders.

In the treatment of schizophrenia, manic episodes, as well as for the prevention of relapses of bipolar disorder, the daily dose can be subsequently adjusted in the range from 5 to 20 mg, taking into account the clinical condition of the individual patient. Dose adjustments beyond the recommended starting dose are recommended only after a thorough clinical review, and should generally occur at intervals of at least 24 hours.

Before discontinuing olanzapine, the dose should be gradually reduced. The maximum daily dose of olanzapine is 20 mg.

Smokers should be prescribed the drug in the same doses as non-smokers. In the presence of more than one factor that can cause a slowdown in metabolism (female sex, elderly age, non-smoking patients), the need to reduce the initial dose to 5 mg/day should be considered. If necessary, it is possible to increase the dose further with caution.

Overdose

Symptoms: tachycardia, agitation / aggressiveness, articulation disorder, extrapyramidal disorders, depression of consciousness of varying severity (from sedation to coma), delirium, convulsions, neuroleptic malignant syndrome, respiratory depression, aspiration, increased or decreased blood pressure, arrhythmias, cardiac and respiratory arrest.

The minimum dose for acute overdose with a fatal outcome was 450 mg, the maximum dose with a favorable outcome (survival) was 1500 mg.

Treatment: gastric lavage, use of activated charcoal, symptomatic treatment, maintenance of respiratory function.

Do not use sympathomimetics (including norepinephrine, dopamine), which are beta-adrenergic agonists (stimulation of these receptors can exacerbate the decrease in blood pressure). Close medical supervision and monitoring should continue until the patient recovers.

Special instructions

While taking antipsychotic medications, improvement in the clinical condition of patients may occur within a few days or weeks. During this period, patients need to be closely monitored.

Dementia-related psychosis and / or behavioral disorders Olanzapine is not approved for use in the treatment of psychosis and/or behavioral disorders associated with dementia, and it is not recommended for use in such patients due to increased mortality and risk of cerebral circulatory disorders. When taking olanzapine in elderly patients with psychosis on the background of dementia, cerebrovascular disorders (stroke, transient ischemic attack), including fatal outcomes, were noted. These patients had previous risk factors (history of cerebrovascular disorders, transient ischemic attacks, hypertension, smoking), as well as concomitant diseases and / or drug use that were associated with cerebrovascular disorders over time.

Olanzapine is not recommended for the treatment of dopamine agonist-related psychoses in patients with Parkinson’s disease.

Neuroleptic malignant syndrome (NMS) Neuroleptic malignant syndrome may develop during treatment with neuroleptics (including olanzapine). Clinical manifestations of NMS include fever, muscle rigidity, changes in mental state, instability of autonomic functions (unstable levels of heart rate and blood pressure, tachycardia, sweating, cardiac arrhythmia). Additional signs may include increased creatine phosphokinase levels, myoglobinuria (rhabdomyolysis), and acute renal failure. If the patient develops symptoms and signs of NMS or develops an unexplained fever without additional clinical manifestations of NMS, all antipsychotic agents, including olanzapine, should be discontinued.

Hyperglycemia and diabetes mellitus There is a higher prevalence of diabetes mellitus in patients with schizophrenia. Very rare cases of hyperglycemia, diabetes mellitus or exacerbation of pre-existing diabetes mellitus, ketoacidosis and diabetic coma have been reported. A causal relationship between antipsychotic drugs and these conditions has not been established. Clinical monitoring of patients with diabetes mellitus or with risk factors for its development is recommended.

Changes in lipid levels If lipid levels change while taking olanzapine, appropriate treatment should be prescribed, especially in patients with dyslipidemia or risk factors for developing fat metabolism disorders.

Anticholinergic activity Despite the fact that olanzapine has anticholinergic activity in vitro, due to the limited clinical experience of olanzapine use in patients with concomitant diseases, caution is recommended when prescribing this drug to patients with prostatic hypertrophy, paralytic intestinal obstruction and other similar conditions.

Liver function Special care should be taken when increasing the activity of hepatic transaminases, ALT and / or ACT in patients with hepatic insufficiency or receiving treatment with potentially hepatotoxic drugs. Monitoring of the patient and, if necessary, dose reduction is required. If hepatitis is detected (including hepatocellular, cholestatic, or mixed liver damage), olanzapine should be discontinued.

Neutropenia Olanzapine should be used with caution in patients with a decrease in the number of leukocytes, including neutrophils; with signs of suppression or toxic impairment of bone marrow function under the influence of drugs (in the anamnesis); with suppression of bone marrow function due to concomitant disease, radio or chemotherapy (in the anamnesis); with hypereosinophilia or myeloproliferative disease. Neutropenia is often observed with the combined use of olanzapine and valproate. Olanzapine use in patients with a history of clozapine-dependent neutrophenia or agranulocytosis it was not accompanied by relapses of these disorders.

Discontinuation of the drug With abrupt discontinuation of olanzapine in very rare cases (

OT interval As with other antipsychotic medications, caution should be exercised during the course of treatment with olanzapine if this drug is prescribed simultaneously with drugs that prolong the QTc interval, especially in elderly patients, patients with congenital QT prolongation syndrome, congestive heart failure, cardiac hypertrophy, hypokalemia, hypomagnesemia, or a family history of QT prolongation.

Concomitant use of other antipsychotics or medications that also prolong the QT interval or cause hypokalemia should be avoided.

Thromboembolism The coincidence in the time of olanzapine use and venous thromboembolism was recorded in rare cases (less than 0.01%). A causal relationship between the symptoms of venous thromboembolism and olanzapine intake has not been established. However, since patients with schizophrenia often have acquired risk factors for venous thromboembolism, it is necessary to identify all possible risk factors for venous thromboembolism, such as immobility of patients, and take preventive measures.

Convulsive seizures Olanzapine should be used with caution in patients who have a history of seizures or are exposed to factors that reduce the threshold of seizure readiness. Seizures are rare in patients receiving olanzapine. Most of these cases have a history of seizures or risk factors for seizures.

Tardive dyskinesia If signs of tardive dyskinesia develop, it is recommended to reduce the dose or cancel olanzapine. Symptoms of tardive dyskinesia may increase or manifest after discontinuation of the drug.

Orthostatic hypotension In clinical trials of olanzapine, orthostatic hypotension was infrequently observed in elderly patients. As with other antipsychotic medications, it is recommended to periodically measure blood pressure in patients over 65 years of age.

Application in pediatrics Olanzapine is not recommended for use in the treatment of children and adolescents. Studies conducted in patients aged 13-17 years revealed various adverse reactions, including weight gain, changes in metabolic parameters, and increased prolactin levels.The long-term outcomes of these events have not been studied and remain unknown.

Lactose This drug contains lactose, so it should not be prescribed to patients with rare hereditary problems of galactose tolerance, hereditary sami lactase deficiency, or glucose-galactose malabsorption. Caution should be exercised when using olanzapine in combination with other centrally acting drugs and ethanol.

Storage conditions

Store at a temperature not exceeding 30 °C. Keep the product out of the reach of children!

Shelf life

3 years

Active ingredient

Olanzapine

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

Schizophrenia, Manic-depressive psychosis